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CAS No. : 578-86-9
MCE 国际站:Liquiritigenin
产品活性:Liquiritigenin是从甘草中分离出的黄烷酮,它是一种高度选择性的雌激素受体β (ERβ) 激动剂,用于活化ERE tk-Luc的 EC50 值为36.5 nM。
研究领域:Vitamin D Related/Nuclear Receptor
作用靶点:Estrogen Receptor/ERR
结构分类:黄酮类 | 二氢黄酮 | 酚类 | 多酚类 | 结构分类
来源:植物 | 豆科 | 甘草
In Vitro: Liquiritigenin produces a dose-response activation of ERE tk-Luc in the U2OS cells transfected with ERβ, but not ERα. Liquiritigenin produces a dose-dependent activation and a time-dependent increase of the CECR6, NKG2E and NKD with ERβ but not with ERα. The ERβ-selectivity of liquiritigenin is due to the selective recruitment of the coactivator steroid receptor coactivator-2 to target genes. Liquiritigenin exhibits similar binding affinities for ERα and ERβ, and causes the recruitment of SRC-2 to target genes selectively in ERβ cells. Pretreatment of MC3T3-E1 cells with liquiritigenin prevents the MG-induced cell death and production of protein adduct, intracellular reactive oxygen species, mitochondrial superoxide, cardiolipin peroxidation, and TNF-α in osteoblastic MC3T3-E1 cells.
In Vivo: In a mouse xenograph model, liquiritigenin does not stimulate uterine size or tumorigenesis of MCF-7 breast cancer cells. Treatment with liquiritigenin significantly reduces the concentrations of pro-inflammatory cytokines including interleukin (IL)-6, IL-1β and tumor necrosis factor (TNF)-α in serum and hippocampus.
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